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Related Concept Videos

Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
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G Protein-coupled Receptors01:15

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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
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G-Protein Gated Ion Channels01:21

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GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
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GPCRs Regulate Adenylyl Cylase Activity01:09

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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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Mechanical Systems01:22

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Mechanical systems are analogous to to electrical networks where springs and masses play similar roles to inductors and capacitors, respectively. A viscous damper in mechanical systems functions similarly to a resistor in electrical networks, dissipating energy. The forces acting on a mass in such systems include an applied force in the direction of motion, counteracted by forces from the spring, a viscous damper, and the mass's acceleration. This interplay of forces is mathematically...
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Mechanically-gated Ion Channels01:12

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Mechanically-gated ion channels are proteins found in eukaryotic and prokaryotic cell membranes that open in response to mechanical stress. Tension, compression, swelling, and shear stress can alter the conformation of the protein, opening a transmembrane channel that allows the passage of ions for signal transmission. In eukaryotes, mechanically-gated channels are distributed in several regions like the neurons, lungs, skin, bladder, and heart, where they play critical roles in numerous...
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Related Experiment Video

Updated: Sep 27, 2025

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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Translating the force-mechano-sensing GPCRs.

Caroline Wilde1, Jakob Mitgau1, Tomáš Suchý1

  • 1Rudolf Schönheimer Institute of Biochemistry, Medical Faculty, Leipzig University, Leipzig, Germany.

American Journal of Physiology. Cell Physiology
|April 13, 2022
PubMed
Summary

Cells sense physical forces through specialized proteins, including G protein-coupled receptors (GPCRs). This review explores how these mechano-sensitive GPCRs respond to mechanical cues like shear stress and cell stretch.

Keywords:
G protein-coupled receptorsadhesion GPCRmechanical forcemechano-sensingsignal transduction

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Area of Science:

  • Cellular Biology
  • Biophysics
  • Physiology

Background:

  • Cells perceive and respond to mechanical forces from their environment.
  • Mechanical cues influence cellular processes like migration, differentiation, and tissue development.
  • Specialized proteins, including ion channels and G protein-coupled receptors (GPCRs), act as mechanosensors.

Purpose of the Study:

  • To review the function of mechano-sensitive GPCRs.
  • To highlight recent advancements in understanding adhesion-type GPCRs.
  • To discuss mechanisms of mechano-activation in GPCRs.

Main Methods:

  • Literature review of studies on mechano-sensitive GPCRs.
  • Focus on specific receptors: angiotensin II type 1, adrenergic, apelin, histamine, parathyroid hormone 1, and orphan receptors.
  • Examination of adhesion-type GPCRs and their mechanosensory roles.

Main Results:

  • GPCRs function as metabotropic force receptors and are significant drug targets.
  • Two primary modes of mechano-activation identified: shear stress and cell swelling/stretch.
  • Exploration of force-from-lipid and force-from-tether models for GPCRs.

Conclusions:

  • Mechano-sensitive GPCRs play a crucial role in cellular responses to physical stimuli.
  • Understanding these receptors offers insights into tissue development, function, and disease.
  • Further research into GPCR mechanotransduction mechanisms is warranted.